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Issue 12, 2006
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Structure–activity studies on a library of potent calix[4]arene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation

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Abstract

Platelet-derived growth factor (PDGF) and its receptor PDGFR are required for tumor growth and angiogenesis, so disruption of the PDGF–PDGFR interaction should lead to starvation of tumors and reduction of tumor growth. Potent PDGF antagonists have been discovered through the synthesis of a series of calix[4]arene-based compounds that are designed to bind to the three-loop region of PDGF. The effect of lower-rim alkylation, linker and number of interacting head groups on the calix[4]arene scaffold on PDGF affinity and cellular activity has been investigated.

Graphical abstract: Structure–activity studies on a library of potent calix[4]arene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation

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Article information


Submitted
01 Nov 2005
Accepted
21 Mar 2006
First published
10 May 2006

Org. Biomol. Chem., 2006,4, 2376-2386
Article type
Paper

Structure–activity studies on a library of potent calix[4]arene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation

H. Zhou, D. Wang, L. Baldini, E. Ennis, R. Jain, A. Carie, S. M. Sebti and A. D. Hamilton, Org. Biomol. Chem., 2006, 4, 2376
DOI: 10.1039/B515483A

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